1239713-09-7Relevant articles and documents
Synthesis and CYP24A1 inhibitory activity of N-(2-(1H-imidazol-1-yl)-2- phenylethyl)arylamides
Aboraia, Ahmed S.,Yee, Sook Wah,Gomaa, Mohamed Sayed,Shah, Nikhil,Robotham, Anna C.,Makowski, Bart,Prosser, David,Brancale, Andrea,Jones, Glenville,Simons, Claire
, p. 4939 - 4946 (2010)
A series of N-(2-(1H-imidazol-1-yl)-2-phenylethyl)arylamides were prepared, using an efficient three- to five-step synthesis, and evaluated for their inhibitory activity against human cytochrome P450C24A1 (CYP24A1) hydroxylase. Inhibition ranged from IC50 0.3-72 μM compared with the standard ketoconazole IC50 0.52 μM, with the styryl derivative (11c) displaying enhanced activity (IC50 = 0.3 μM) compared with the standard, providing a useful preliminary lead for drug development.